The Oral Bioavailability of <i>Trans</i>‐Resveratrol from a Grapevine‐Shoot Extract in Healthy Humans is Significantly Increased by Micellar Solubilization

Calvo-Castro, Laura A.; Schiborr, Christina; David, Franziska; Ehrt, Heidi; Voggel, Jenny; Sus, Nadine; Behnam, Dariush; Bosy‐Westphal, Anja; Frank, Jan

doi:10.1002/mnfr.201701057

Cited by 58 publications

(40 citation statements)

References 34 publications

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“…Thus the two issues of resveratrol bioavailability and resistance exercise protocol should be examined further in order to understand their combinational benefits and mechanisms. The oral bioavailability of resveratrol in humans is quite limited, but may be increased significantly without any treatment-related adverse effects through the use of a liquid micellar formulation [ 39 ]. The dose in current animal studies could be further converted to human dose according to the conversion factor of 12.3-fold by body surface area difference, suggested by US Food and Drug Administration [ 40 ].…”

Section: Discussionmentioning

confidence: 99%

The Synergistic Effects of Resveratrol combined with Resistant Training on Exercise Performance and Physiological Adaption

et al. 2018

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The comprehensive studies done on resveratrol (RES) support that this polyphenol has multiple bioactivities and is widely accepted for dietary supplementation. Furthermore, regular exercise is known to have benefits on health and is considered as a form of preventive medicine. Although the vast majority of prior studies emphasize the efficacy of aerobic exercise in promoting physiological adaptions, other types of exercise, such as resistance exercise and high-intensity interval training (HIIT), may achieve similar or different physiological outcomes. Few studies have looked into the effectiveness of a combinational, synergistic approach to exercise using a weight-loading ladder climbing animal platform. In this study, ICR mice were allocated randomly to the RES and training groups using a two-way ANOVA (RES × Training) design. Exercise capacities, including grip strength, aerobic performance, and anaerobic performance, were assessed and the physiological adaptions were evaluated using fatigue-associated indexes that were implemented immediately after the exercise intervention. In addition, glycogen levels, muscular characteristics, and safety issues, including body composition, histopathology, and biochemistry, were further elucidated. Synergistic effects were observed on grip strength, anaerobic capacities, and exercise lactate, with significant interaction effects. Moreover, the training or RES may have contributed significantly to elevating aerobic capacity, tissue glycogen, and muscle hypertrophy. Toxic and other deleterious effects were also considered to evaluate the safety of the intervention. Resistance exercise in combination with resveratrol supplementation may be applied in the general population to achieve better physiological benefits, promote overall health, and promote participation in regular physical activities.

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Section: Discussionmentioning

confidence: 99%

The Synergistic Effects of Resveratrol combined with Resistant Training on Exercise Performance and Physiological Adaption

et al. 2018

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“…These include several delivery systems such as the encapsulation of RES in lipid nanocarriers or liposomes, emulsions, micelles, insertion into polymeric nanoparticles, solid dispersions, and nanocrystals [59,60]. For example, the bioavailability of RES from the grapevine shoot extract Vineatrol30 has been significantly increased using a liquid micellar formulation, without any treatment-related adverse effects, making it a suitable system for improved supplementation [61]. On the other hand, the bioavailability of RES delivered through oral mucosa may be significantly higher than by swallowing, as determined by the fraction of the initial RES intake in the blood and, under metabolized form, in the urine [62].…”

Section: Bioavailability Of Resveratrol and Potential Side Effectsmentioning

confidence: 99%

The Plant-Derived Compound Resveratrol in Brain Cancer: A Review

et al. 2020

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Despite intensive research, malignant brain tumors are among the most difficult to treat due to high resistance to conventional therapeutic approaches. High-grade malignant gliomas, including glioblastoma and anaplastic astrocytoma, are among the most devastating and rapidly growing cancers. Despite the ability of standard treatment agents to achieve therapeutic concentrations in the brain, malignant gliomas are often resistant to alkylating agents. Resveratrol is a plant polyphenol occurring in nuts, berries, grapes, and red wine. Resveratrol crosses the blood‒brain barrier and may influence the central nervous system. Moreover, it influences the enzyme isocitrate dehydrogenase and, more importantly, the resistance to standard treatment via various mechanisms, such as O6-methylguanine methyltransferase. This review summarizes the anticancer effects of resveratrol in various types of brain cancer. Several in vitro and in vivo studies have presented promising results; however, further clinical research is necessary to prove the therapeutic efficacy of resveratrol in brain cancer treatment.

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“…To date, several formulation strategies such as amorphous solid dispersions, composite nanoparticles, emulsions, liposomes, polymeric micelles, self-emulsifying drug delivery systems, and solid lipid nanoparticles have been investigated to resolve this problem [10][11][12][13][14][15][16][17][18][19]. In addition, the enhanced oral bioavailability in humans has been reported with lipid formulation, micellar liquid formulation, and microparticles mixed with a liquid formulation [20][21][22]. Previously, the area under the plasma concentration versus time curve (AUC) and maximum plasma concentration (C max ) values obtained after oral administration at a dose of 40-mg trans-resveratrol were approximately 10-fold and 8.5-fold higher in the capsule containing solubilized resveratrol in polysorbate 20 and polyglyceryl-3-dioleate mixture than in powder capsule (original powder), respectively [20].…”

Section: Introductionmentioning

confidence: 99%

“…Previously, the area under the plasma concentration versus time curve (AUC) and maximum plasma concentration (C max ) values obtained after oral administration at a dose of 40-mg trans-resveratrol were approximately 10-fold and 8.5-fold higher in the capsule containing solubilized resveratrol in polysorbate 20 and polyglyceryl-3-dioleate mixture than in powder capsule (original powder), respectively [20]. In a case study using capsules containing solubilized resveratrol in polysorbate 80, polysorbate 20, and medium chain triacylglycerol mixtures, the intake of a liquid micellar formulation containing 30 mg trans-resveratrol produced higher AUC (5.0-fold increase) and C max (10.6-fold increase) than the equivalent dose of the original powder [21]. In a human pharmacokinetic study using a suspension prepared by mixing resveratrol powder and the liquid formulation (docusate sodium solution and distilled water) at a daily dose of 5.0 g trans-resveratrol, the oral bioavailability of the micronized powder (particle size less than 5 µm) was significantly higher than that of the nonmicronized powder, with approximately 3.6-fold increases in the C max values at 14 days [22].…”

Section: Introductionmentioning

confidence: 99%

Pure Trans-Resveratrol Nanoparticles Prepared by a Supercritical Antisolvent Process Using Alcohol and Dichloromethane Mixtures: Effect of Particle Size on Dissolution and Bioavailability in Rats

Park

Lee

et al. 2020

Antioxidants

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The aim of this study was to prepare pure trans-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) using a supercritical antisolvent (SAS) process with alcohol (methanol or ethanol) and dichloromethane mixtures. In addition, in order to investigate the effect of particle size on the dissolution and oral bioavailability of the trans-resveratrol, two microparticles with different sizes (1.94 µm and 18.75 µm) were prepared using two different milling processes, and compared to trans-resveratrol nanoparticles prepared by the SAS process. The solid-state properties of pure trans-resveratrol particles were characterized. By increasing the percentage of dichloromethane in the solvent mixtures, the mean particle size of trans-resveratrol was decreased, whereas its specific surface area was increased. The particle size could thus be controlled by solvent composition. Trans-resveratrol nanoparticle with a mean particle size of 0.17 µm was prepared by the SAS process using the ethanol/dichloromethane mixture at a ratio of 25/75 (w/w). The in vitro dissolution rate of trans-resveratrol in fasted state-simulated gastric fluid was significantly improved by the reduction of particle size, resulting in enhanced oral bioavailability in rats. The absolute bioavailability of trans-resveratrol nanoparticles was 25.2%. The maximum plasma concentration values were well correlated with the in vitro dissolution rate. These findings clearly indicate that the oral bioavailability of trans-resveratrol can be enhanced by preparing pure trans-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) by the SAS process. These pure trans-resveratrol nanoparticles can be applied as an active ingredient for the development of health supplements, pharmaceutical products, and cosmetic products.

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The Oral Bioavailability of Trans‐Resveratrol from a Grapevine‐Shoot Extract in Healthy Humans is Significantly Increased by Micellar Solubilization

Abstract: The oral bioavailability of trans-resveratrol from the grapevine-shoot extract Vineatrol30 was significantly increased using a liquid micellar formulation, without any treatment-related adverse effects, making it a suitable system for improved supplementation of trans-resveratrol.

Cited by 58 publications

References 34 publications

The Synergistic Effects of Resveratrol combined with Resistant Training on Exercise Performance and Physiological Adaption

The Synergistic Effects of Resveratrol combined with Resistant Training on Exercise Performance and Physiological Adaption

The Plant-Derived Compound Resveratrol in Brain Cancer: A Review

Pure Trans-Resveratrol Nanoparticles Prepared by a Supercritical Antisolvent Process Using Alcohol and Dichloromethane Mixtures: Effect of Particle Size on Dissolution and Bioavailability in Rats

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